Investigation of antioxidant properties of some 6-(alpha-aminobenzyl)thiazolo[3,2-b]-1,2,4-triazole-5-ol compounds.
Promising antiinflammatory activity together with low ulcerogenic properties of some Michael addition products of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones which have been synthesized in our previous study, prompted us to investigate their antioxidant properties. Since compound Ib has both antioxidant and antiinflammatory activities beside the lowest ulcerogenic incidence, it was selected for investigation of its inhibitory effect on various cyclooxygenase ezymes. It was found that while it did not inhibit cyclooxygenase-1 (COX-1) enzyme, there was a small inhibitory effect (17%) on COX-2 enzyme. We concluded that the diminished harmful effects on the stomach of this novel antiinflammatory compound were related to its antioxidant properties since it is ineffective on COX-1 enzyme. In conclusion, the compounds having both antioxidant and antiinflammatory activities with a lack of COX-1 enzyme inhibitory effect may improve the gastrointestinal safety profile of such compounds.
Aktay
Goknur
G
Department of Pharmacology, Faculty of Pharmacy, Inonu University, 44280, Malatya, Turkey. gaktay@inonu.edu.tr
Tozkoparan
Birsen
B
Ertan
Mevlut
M
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051545:Cyclooxygenase 1 / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D000431:Ethanol / Q000494:pharmacology; D005767:Gastrointestinal Diseases / Q000139:chemically induced / Q000517:prevention & control; D020128:Inhibitory Concentration 50; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D051379:Mice; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology; D013997:Time Factors; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D001593:Benzyl Compounds; D016861:Cyclooxygenase Inhibitors; D014230:Triazoles; C045575:1,2,4-triazole; D000431:Ethanol; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2